Studies in Enteric Anthelmintics: Activity Profile of Prodrug of a Bisbenzimidazole [1]

A. M. Khan, Suman Gupta, J. C. Katiyar, Sudhir K. Singh, V. L. Sharma, Satyavan Sharma, A. P. Bhaduri

Research output: Contribution to journalArticlepeer-review

5 Scopus citations

Abstract

The comparative anthelmintic activity of a possible prodrug, 2,2' ‘-dicarbomethoxyamino-5,5’-dibenzimidazolyl methanol (2) with its parent compound 2,2' ‘-dicarbomethoxyamino-5,5’-dibenzimidazolyl ketone (1) and the reference drug mebendazole (3a) is reported. At a dose of 25 mg/kg, compound 2 was 100% effective against Ancylostoma ceylanicum in hamsters. Compound 2 also exhibited a similar order of activity against Syphacia obvelata, Hymenolepis nana and H. diminuta at a dose of 100 mg/kg. The drug exhibited lethal effects against metamorphic forms of A. ceylanicum at a dose of 100 mg/kg. However the trichostrongylids, Nippostrongylus brasiliensis remained unaffected up to a dose of 250 mg/kg of 2. Both 1 and 3 a exhibited' ‘ inferior activity than 2 except against adult A. ceylanicum. The activity of 1 and 2 has been explained on the basis of their ability to resist systemic hydrolysis resulting in higher concentration of the active drug in biophase.

Original languageEnglish
Pages (from-to)673-677
Number of pages5
JournalZeitschrift fur Naturforschung - Section C Journal of Biosciences
Volume46
Issue number7-8
DOIs
StatePublished - 1 Jan 1991
Externally publishedYes

Keywords

  • Anthelmintic Activity
  • Bisbenzimidazole
  • Comparative Efficacy
  • Prodrug

ASJC Scopus subject areas

  • General Biochemistry, Genetics and Molecular Biology

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